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非苯二氮䓬类抗焦虑药恩西拉嗪及相关化合物的化学与药理学

Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.

作者信息

Engel J, Fleischhauer I, Jakovlev V, Kleemann A, Kutscher B, Nickel B, Rauer H, Werner U, Szelenyi I, Johanson C E

机构信息

ASTA Pharma AG, Frankfurt, FRG.

出版信息

J Med Chem. 1990 Nov;33(11):2976-81. doi: 10.1021/jm00173a012.

Abstract

In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized. These are 1-(3,4,5-trimethoxyphenoxy)-3-[4-(2-methoxyphenyl)piperazinyl]prop an-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity. Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected. Enciprazine was selected for clinical investigations.

摘要

在对镇静剂的研究过程中,合成了新型非苯二氮䓬类化合物。这些化合物是1-(3,4,5-三甲氧基苯氧基)-3-[4-(2-甲氧基苯基)哌嗪基]丙-2-醇(国际非专利药品名称:恩西拉嗪)及其衍生物,为评估其对中枢神经系统的活性,对它们进行了药理筛选。检测到具有显著抗攻击和抗焦虑特性但无成瘾潜力的化合物。恩西拉嗪被选用于临床研究。

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